Assay Detail
Binding
CHEMBL862543
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Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological studies of a new series of 5-heteroarylcarbamoylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists. Influence of the heteroaryl substituent on binding affinity and molecular modeling investigations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.48 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383714 | — | — | 1 | 6.68 |
| CHEMBL203797 | — | — | 1 | 6.64 |
| CHEMBL534489 | — | — | 1 | 6.61 |
| CHEMBL332091 | — | — | 1 | 6.58 |
| CHEMBL534936 | — | — | 1 | 6.58 |
| CHEMBL203660 | — | — | 1 | 6.48 |
| CHEMBL118923 | — | — | 1 | 6.45 |
| CHEMBL383689 | — | — | 1 | 6.40 |
| CHEMBL203060 | — | — | 1 | 6.26 |
| CHEMBL203998 | — | — | 1 | 6.10 |
| CHEMBL382357 | — | — | 1 | - |
| CHEMBL204753 | — | — | 1 | - |
| CHEMBL204128 | — | — | 1 | - |
| CHEMBL382665 | — | — | 1 | - |
| CHEMBL381123 | — | — | 1 | - |
| CHEMBL203054 | — | — | 1 | - |
| CHEMBL262987 | — | — | 1 | - |
| CHEMBL203506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383714 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL203797 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL534489 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL332091 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL534936 | — | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL203660 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL118923 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL383689 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL203060 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL203998 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL382357 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL204753 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL204128 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL382665 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL381123 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL203054 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL262987 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL203506 | — | Ki | > | 1000.0 | nM | - |